Oxygen Double Bonded And Nitrogen Bonded Directly To The Same Carbon Patents (Class 536/53)
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Publication number: 20120095187Abstract: Disclosed are a novel cyanine compound, represented by the following Formula 1, for labeling biomolecules, and a method for preparing the same. wherein R1, R2, R3, R4, B, m and n are defined as above.Type: ApplicationFiled: April 2, 2010Publication date: April 19, 2012Applicants: DKC CORPORATION, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Dong Jin Kim, Young Soo Kim, Jong Joo Na, Jin Woo Park, Ki Won Kim
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Publication number: 20120095203Abstract: The invention relates to a silane compound including a cycloalkyne functionality, to a method for functionalising a solid substrate, and to the solid substrate thus produced. The silane compound of the invention corresponds to the formula X-E-A-Z where X is a silyl group, E is an organic spacer group, A is a single bond or a —CONH—, —NHCO—, —OCH2CONH—, —NHCOCH2O—, —0— or —S— group, and Z is a cycloalkyne or heterocycloalkyne with at least 8 members. The invention is particularly suitable for use in the field of medicine.Type: ApplicationFiled: March 16, 2010Publication date: April 19, 2012Applicant: Commissariat A L'Energie Atomique Et Aux Ene AltInventors: Aude Bernardin, Guillaume Delapierre, Antoine Hoang, Isabelle Texier-Nogues
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Patent number: 8158763Abstract: An asparagine-linked ?2,3-oligosaccharide having undeca- to hepta-saccharides, an asparagine-linked ?2,6-oligosaccharide having undeca- to hepta-saccharides and containing fluorine and an asparagine-linked oligosaccharide derivative containing at least one fucose in N-acetylglucosamine on the nonreducing terminal side of an asparagine-linked oligosaccharide wherein the asparagine has amino group protected with a lipophilic protective group, and a process for producing these compounds.Type: GrantFiled: October 25, 2007Date of Patent: April 17, 2012Assignees: Otsuka Chemical Co. Ltd.Inventors: Yasuhiro Kajihara, Kazuaki Kakehi, Kazuhiro Fukae
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Patent number: 8153135Abstract: Disclosed is a method of producing a polysaccharide-polypeptide conjugate by reacting a polysaccharide with a polypeptide which contains at least one free amino group, wherein a polysaccharide carrier comprising vicinal hydroxyl groups is oxidized under ring opening to create vicinal aldehyde groups and is reacted with one or more base-instable antigenic polypeptide(s) containing at least one free amino group, the polypeptide(s) being bound directly to the polysaccharide carrier via at least one azomethine bond.Type: GrantFiled: September 13, 2005Date of Patent: April 10, 2012Inventors: Hans Loibner, Helmut Eckert
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Patent number: 8153440Abstract: Various methods for altering surface characteristics of a microsphere are provided. One method includes coupling an enolic acid to the microsphere to modify the surface characteristics of the microsphere. The surface characteristics may include charge density and/or pKa. A reagent can be coupled to the microsphere via the enolic acid. The reagent may include a biomolecule. The modified surface characteristics may increase a stability of the reagent when the reagent is coupled to the microsphere. The modified surface characteristics may also improve performance of an assay carried out with the microsphere. Another embodiment relates to a microsphere that includes an enolic acid coupled to a polymer core of the microsphere such that the enolic acid modifies surface characteristics of the microsphere. A reagent can be coupled to the microsphere via the enolic acid.Type: GrantFiled: December 16, 2010Date of Patent: April 10, 2012Assignee: Luminex CorporationInventors: Ananda G. Lugade, Kurt D. Hoffacker
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Publication number: 20120077760Abstract: The present invention relates to novel pharmaceutically acceptable salts of sitagliptin, to processes for their preparation and to pharmaceutical compositions containing them.Type: ApplicationFiled: February 10, 2010Publication date: March 29, 2012Applicant: LEK Pharmaceuticals D.D.Inventors: Lovro Selic, Ivan Plantan
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Patent number: 8143391Abstract: The present invention provides a water-soluble modified HA practically used as a drug carrier and a production method thereof. The present invention provides: a water-soluble modified hyaluronic acid, the residence time in blood of which is elongated to a practical level, which is produced by introducing a substituent into the carboxy group of the glucuronic acid of hyaluronic acid or a derivative thereof, via an amide bond, at a lower limit of an introduction ratio of 5 mole % or more, using a BOP condensing agent in an aprotic polar solvent; and a production method thereof. Moreover, by cross-linking the modified hyaluronic acid, the present invention provides a hyaluronic acid gel capable of extremely long drug sustained-release even at the same cross-linking functional group introduction ratio as that of the conventionally known gel.Type: GrantFiled: September 7, 2005Date of Patent: March 27, 2012Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kenji Yasugi, Teruo Nakamura, Tsuyoshi Shimoboji, Mika Sato
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Publication number: 20120071441Abstract: The present invention relates to a process of synthesis of ?-sialyl oligosaccharides and in particular of 6?-sialyllactose and its salts comprising a step of coupling by Koenigs-Knorr reaction under conditions that allow its use on an industrial scale.Type: ApplicationFiled: April 6, 2010Publication date: March 22, 2012Applicant: INALCO S.P.A.Inventors: Giancarlo Tamerlani, Ilaria Lombardi, Debora Bartalucci, Andrea Danesi, Liana Salsini, Marco Manoni, Giovanni Cipolletti
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Patent number: 8129518Abstract: Provided are synthetic polysaccharide antigens (SPAs) with anti-inflammatory or inflammatory immunomodulatory properties, depending on their structure. Also provided are compositions comprising these SPAs, and methods of using these SPAs and compositions to either prevent or treat inflammatory pathologies, or diseases or conditions susceptible to treatment with inflammatory immunomodulators, by using appropriate SPAs.Type: GrantFiled: September 15, 2004Date of Patent: March 6, 2012Assignee: Eli Lilly and CompanyInventors: Larry Chris Blaszczak, John Astor Cleveland, Jr., Kathleen Ann Taylor, Neil Thomas Blackburn, Angelika Regina Kraft, Charles Ellis Cohen
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Publication number: 20120053132Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: November 1, 2011Publication date: March 1, 2012Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Publication number: 20120052042Abstract: The present disclosure relates to amphiphilic compounds, self assembling compositions formed from the amphiphilic compounds and methods of making such compositions.Type: ApplicationFiled: February 22, 2010Publication date: March 1, 2012Inventors: Sébastien Ladet, Philippe Gravagna
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Patent number: 8124757Abstract: The disclosed is thiol-modified macromolecule derivatives having the general formula of (I) or (II), as well as the disulfide bond cross-linked materials and the thiol-reactive crosslinker cross-linked materials, wherein R1 and R2 are alkylene groups, substituted alkylene groups, aromatic groups or polyether groups and the like, respectively. R1 and R2 may have same or different chemical structure, and P is a residue of a macromolecule with side carboxyl group. The thiol-modified macromolecule derivative has a molecular weight of from 1000 to 5,000,000. The thiol-modified macromolecule derivative having the general formula of (I) or (II) of the present invention has a side chain with flexible chemical structure and adjustable properties, and has a number of advantages, such as mild reaction condition, high production yield, high degree of modifying, and the controllable modifying degree and so on.Type: GrantFiled: September 29, 2007Date of Patent: February 28, 2012Assignee: Bioregen Biomedical (Changzhou) Co., Ltd.Inventor: Chan Song
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Publication number: 20120045566Abstract: An oligosaccharide ingredient comprising glycosylated amino acids and peptides of the general formula RnSacm where R is an amino acid residue, Sac is a monosaccharide selected from the group comprising N-acetyl-neuraminic acid, N-acetyl galactosamine and galactose, n has a value between 1 and 10 with the proviso that if n has the value 1 R is a threonine residue or a serine residue and if n has a value between 2 and 10 the peptide contains at least one threonine or serine residue, m has a value between 2 and 4 and at least 20 mol % of the ingredient is N-acetyl-neuraminic acid.Type: ApplicationFiled: March 4, 2009Publication date: February 23, 2012Applicant: NESTEC S.A.Inventors: Norbert Sprenger, Rafael Berrocal, Marie-Claire Fichot
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Publication number: 20120046737Abstract: Implantable biocompatible polymeric medical devices include a substrate with an acid or base-modified surface which is subsequently modified to include click reactive members.Type: ApplicationFiled: February 19, 2010Publication date: February 23, 2012Inventors: Nadya Belcheva, Ferass Abuzaina, Amin Elachchabi, Mbiya Kapiamba, Ahmad Robert Hadba
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Publication number: 20120035128Abstract: Disclosed are a polysaccharide derivative obtained by substituting some of the carboxyl groups of a carboxy polysaccharide with —NH—X—CO—Y—Z; and a hydrogel thereof. Here, X is a C1-10 hydrocarbon group, Y is a polyalkylene oxide having oxygen atoms at both ends, and Z is a C1-24 hydrocarbon group or —CO—R2, with R2 being a C1-23 hydrocarbon group. The hydrogel has excellent viscoelasticity and can be injected into a predetermined location with an injection device such as a syringe, and thus can be advantageously used as a medical gel or an adhesion barrier.Type: ApplicationFiled: April 19, 2010Publication date: February 9, 2012Applicant: TEIJIN LIMITEDInventors: Hiroaki Kaneko, Masaya Ito
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Publication number: 20120034637Abstract: The invention relates to a method and a kit for the detection of Trichomonas infection by detecting N-acetyl-?-D-hexosaminidase activity. The invention also relates to a method and a kit for selective detection of presence of Trichomonas or Candida infection.Type: ApplicationFiled: January 27, 2010Publication date: February 9, 2012Inventors: Zeyu Wang, Hongyun Yang, Guangyu Fu, Xuewei Wu, Chaojie Feng, Yang Yang, Jingjing Yang, Yuanyuan Xie, Yehuan Zheng, Guilin Li, Fan Yang
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Publication number: 20120020958Abstract: The present invention relates to methods and compositions for the treatment and/or prevention of diseases such as allergic diseases and inflammatory bowel diseases comprising one or more FIBCD1 binding molecules or pharmaceutically acceptable salts, esters, and amides thereof and optionally one or more non-FIBCD1 binding molecules or pharmaceutically acceptable salts, esters, and amides thereof; as well as the use of such pharmaceutical composition for the prevention and/or treatment of diseases such as allergic diseases and inflammatory bowel diseases. FIBCD1 is herein defined as either a transmembrane receptor, the corresponding DNA or the corresponding mRNA as defined by SEQ ID No. 1, 2 and 3 as well as homologous thereof.Type: ApplicationFiled: December 30, 2008Publication date: January 26, 2012Applicant: Dansk UniversitetInventors: Uffe Holmskov, Anders Schlosser
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Patent number: 8093374Abstract: The present invention discloses a bismuth hyaluronate, characterized in that the bismuth content is from 0.5% to 40%, and the glucuronate content is from 20% to 45%, based on dry weight. Also provided is a method for the preparation of said bismuth hyaluronate comprising reaction of a soluble hyaluronate salt with a bismuth salt in a basic aqueous solution, followed by steps of precipitation, filtration, desalting, dehydrating and drying to obtain the product. Further disclosed is the use of the bismuth hyaluronate in the manufacture of a medicament or health foods for preventing and treating gastrointestinal disorders, in particular ulcerous disorders of the GI tract. It has been proven in animal experiments to show a better therapeutic effect than products of the same type.Type: GrantFiled: December 1, 2006Date of Patent: January 10, 2012Inventors: Peixue Ling, Yanli He, Jianying Chen, Jie Liu, Tianmin Zhang, Xueping Guo, Yan Jin
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Publication number: 20120004405Abstract: The present invention relates to a compound which is characterized by the formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof, wherein the ring systems A and B are independently selected from a monosaccharide, aryl (preferably phenyl), a heteroaryl or cycloalkyl (preferably cyclohexan), preferably with all substituents in equatorial configurations; R1 is independently selected from alkyl (preferably C1 to C6), a substituted or unsubstituted phenyl, preferably CH3; R2 is H, alkyl (preferably C1 to C6), a carbohydrate in a glycosidic ?-linkage, preferably H; R3, R4, R5, and R6 are independently selected from H, (OH) hydroxy, alkyl preferably C1 to C6, alkoxy (preferably C1 to C6), amino, alkylamino (preferably C1 to C6), halogen, benzylamino, or benzoylamino; X is O, NH, alkylamino (NR), CO, S; and Y is O, NH, alkylamino (NR), CO, S.Type: ApplicationFiled: December 14, 2009Publication date: January 5, 2012Inventor: Peter Prehm
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Patent number: 8088916Abstract: An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases. There is provided a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases, wherein methotrexate is conjugated with a carboxyl group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids.Type: GrantFiled: March 4, 2005Date of Patent: January 3, 2012Assignee: Denki Kagaku Kogyo Kabushiki KaishaInventors: Hitoshi Ikeya, Tadashi Morikawa, Koichi Takahashi, Tatsuya Tamura, Akira Okamachi, Takenori Ishizawa, Haruhiko Sato, Yoshinobu Higuchi
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Publication number: 20110319592Abstract: The present invention relates to a novel process for the purification of antibodies, e.g. monoclonal antibodies. The process utilizes an affinity resin comprising a solid phase material having immobilized thereto one or more low-molecular weight synthetic ligands. The affinity resins enable the separation of antibodies from even closely related proteins.Type: ApplicationFiled: November 13, 2009Publication date: December 29, 2011Applicant: Novo Nordisk A/SInventors: Phaedria Marie St. Hilaire, Anders Laerke Nielsen
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Publication number: 20110306574Abstract: The present invention relates to blood group A/B/H determinant on Type 1 Core glycosphingolipids chains as recognition point for the FedF protein of F18-fimbriated Enterotoxigenic and verotoxinogenic Escherichia coli and the use of compounds comprising such determinants for the treatment of F18? E. coli infections in pigs and in screening methods.Type: ApplicationFiled: September 30, 2009Publication date: December 15, 2011Applicant: GHENT UNIVERSITYInventors: Annelies Coddens, Eric Cox, Susann Eva Teneberg
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Publication number: 20110306759Abstract: The present invention provides 4-isopropylphenyl glucitol compounds which have no tendency to accumulate in the body and which inhibit SGLT1 activity to suppress postprandial hyperglycemia (or impaired glucose tolerance) through suppression of glucose absorption in the small intestine, whereby the compounds, for example, can suppress the onset of diabetes and metabolic syndrome or can treat these diseases. A 4-isopropylphenyl glucitol compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents a hydrogen atom, etc., R2 represents a methyl group, etc., R3 represents a C1-4 alkyl group substituted with an amino group(s), etc., and R4 represents a hydrogen atom, etc.Type: ApplicationFiled: February 23, 2010Publication date: December 15, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Hiroyuki Kakinuma, Yohei Kobashi, Tomomichi Chonan, Takahiro Oi, Fumiyasu Shiozawa, Yuki Iwata, Kenichi Kawabe
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Publication number: 20110301109Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.Type: ApplicationFiled: December 10, 2009Publication date: December 8, 2011Applicants: TOPHARMAN SHANGHAI CO., LTD.Inventors: Zheng Liu, Jianfeng Li, Xiaojun Yang, Zhen Wang, Jinfeng Zhang, Yi Zhu, Guanghui Tian, Qing Jin, Jingkang Shen, Weiliang Zhu, Hualiang Jiang, Jingshan Shen
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Publication number: 20110301083Abstract: Conjugates which comprise a drug and a ligand which includes a first saccharide; wherein the conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the conjugate is sensitive to serum concentration of a second saccharide. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.Type: ApplicationFiled: January 27, 2010Publication date: December 8, 2011Inventors: Todd C. Zion, Thomas M. Lancaster
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Patent number: 8071756Abstract: A photocrosslinked polysaccharide pseudo-sponge exhibiting a low swelling property and a high degradation ability in vivo while retaining a suitable strength. The polysaccharide pseudo-sponge is produced by a crosslinking reaction of a photoreactive polysaccharide obtained by introducing a photoroactive group into a polysaccharide, and exhibits a low swelling property and a blue dextran-low dyaffinity.Type: GrantFiled: September 10, 2004Date of Patent: December 6, 2011Assignee: Seikagaku CorporationInventor: Tomoya Sato
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Publication number: 20110294749Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: ApplicationFiled: June 28, 2011Publication date: December 1, 2011Applicant: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110294998Abstract: The present invention relates to novel compositions comprising polymeric moieties covalently attached to therapeutic agents, wherein the therapeutic agent is attached to the polymeric moiety through a tether. By selecting from a variety of tether groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein.Type: ApplicationFiled: August 4, 2011Publication date: December 1, 2011Applicant: CERULEAN PHARMA INC.Inventors: Mark E. Davis, Jungyeon Hwang, Tianyi Ke, Ching-Jou Lim, Thomas Schluep
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Publication number: 20110280914Abstract: Described herein are composites useful in tissue and organ engineering. In one aspect, the composite comprises the reaction product between a macromolecule comprising at least one thiol group and a gold nanoparticle. The thiolated macro-molecule crosslinks with the gold nanoparticle to produce a composite that is useful in anchoring cells. The composites can be used to form multi-layer 3-D structures, where the cells in each layer can aggregate and fuse with one another to form tissues and organs.Type: ApplicationFiled: December 17, 2009Publication date: November 17, 2011Applicant: University of Utah Research FoundationInventors: Glenn D. Prestwich, Aleksander Skardel, Jianxing Zhang
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Publication number: 20110281819Abstract: A low-molecular-weight polysulfated hyaluronic acid derivative useful for prevention and/or treatment of an allergic disease. An agent for prevention and/or treatment of an allergic disease selected from pollinosis, allergic rhinitis, allergic conjunctivitis, atopic dermatitis, and asthma, represented by the following general formula (IA) or (IB); wherein n represents a number of 0 to 15; R?s each independently represent a hydrogen atom or an SO3H group etc.Type: ApplicationFiled: February 1, 2010Publication date: November 17, 2011Applicants: OTSUKA PHARMACEUTICAL CO., LTD., OTSUKA CHEMICAL CO., LTD.Inventors: Kazuaki Kakehi, Hiroaki Asai, Naohiro Hayashi, Satoshi Shimizu, Fumitaka Goto, Yasuo Koga, Takahiro Tomoyasu, Takao Taki, Yusuke Kato, Satoru Nakazato, Junji Takaba, Atsushi Azuma, Wakako Hirano, Kazunari Izumi, Minoru Kashimoto, Yoko Sakamoto, Takashi Hayashi, Masaru Nishida
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Publication number: 20110281817Abstract: Methods for producing hyaluronic acid are described, including altering the activity in Streptococcus cells of one or more enzymes and/or altering the amount of available substrates or substrate precursors.Type: ApplicationFiled: August 29, 2008Publication date: November 17, 2011Applicants: SUGAR INDUSTRY INNOVATION PTY. LTD., THE UNIVERSITY OF QUEENSLANDInventors: Lars Keld Nielsen, Wendy Chen, Esteban Stefane Marcellin Saldana
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Publication number: 20110282028Abstract: The invention provides a method of identifying an inhibitor of LtaS comprising: (a) providing bacteria which comprise a mutation in the mbl gene or homologue thereof; (b) culturing the bacteria of (a) in the presence of a test substance under conditions of low magnesium; (c) monitoring the growth of the bacteria; wherein growth or more rapid growth of the bacteria compared to growth in the absence of the test substance is indicative that the test substance is an inhibitor of LtaS.Type: ApplicationFiled: December 4, 2009Publication date: November 17, 2011Applicant: UNIVERSITY OF NEWCASTLE UPON TYNEInventors: Jeffery Errington, Kathrin Schirner
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Publication number: 20110274646Abstract: The present invention relates to a combination of a hyaluronan oligomer and/or polymer and a factor capable of mobilizing stem cells. The present invention also relates to a method for altering the relative amounts of blood cells and/or the types of blood cells in a subject by administering the combination to the subject. Further, the present invention relates to a method for mobilizing stem cells to the bloodstream of a subject by administering the combination to the subject. Additionally, the present invention relates to a hyaluronan oligomer and/or polymer.Type: ApplicationFiled: May 6, 2011Publication date: November 10, 2011Applicants: Glykos Finland Oy, Suomen Punainen Risti VeripalveluInventors: Johanna Nystedt, Heidi Anderson, Tero Satomaa, Jari Natunen, Jari Helin, Juhani Saarinen
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Publication number: 20110269700Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts thereof, and to formulations and uses of the compounds of formula (I) in the treatment of metabolic disorders.Type: ApplicationFiled: September 17, 2009Publication date: November 3, 2011Inventors: P. Venkata Palle, Debnath Bhuniya, Dumbala Srinivas Reddy, Suresh Eknath Kurhade
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Publication number: 20110257123Abstract: A hyaluronic acid derivative, and methods of producing and using said derivative, the derivative comprising n repeating units and having the general structural formula (I), wherein, in at least one repeating unit, one or more of R1, R2, R3, R4 comprises an etherbound aryl/alkyl sulfone having the general structural fomula (II), wherein R comprises an alkyl- or aryl-group, and otherwise R1, R2, R3, R4 are hydroxyl groups, OH.Type: ApplicationFiled: March 2, 2007Publication date: October 20, 2011Applicant: Novozymes Biopolymer A/SInventors: Corinne Eenschooten, Morten Wurtz Christensen
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Publication number: 20110251363Abstract: The invention relates to stereoregular ROMP polymers, the monomers used to make them, and the processes used to convert the monomers to the polymers.Type: ApplicationFiled: July 17, 2007Publication date: October 13, 2011Inventors: Nicole S. Sampson, Kathlyn A. Parker
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Publication number: 20110243851Abstract: There is provided a glucose-PEG conjugate comprising a PEG moiety conjugated to a linear glucose moiety at the C1 position of the glucose moiety. The glucose-PEG conjugate may be used to reduce glucose transport into a cell and may be used to treat a proliferative disorder.Type: ApplicationFiled: December 11, 2009Publication date: October 6, 2011Applicant: Agency for Science, Technology and ResearchInventors: Karthikeyan Narayanan, Andrew Chwee Aun Wan, Jackie Y. Ying, Nandanan Erathodiyil
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Publication number: 20110237529Abstract: The invention provides adenosine analog compounds that act at P2Y receptors, e.g., the P2Y2 receptor, including pharmaceutical compositions; and uses thereof to treat or prevent diseases associated with that receptor, e.g., disorders relating to mucus secretion, such as cystic fibrosis, chronic obstructive pulmonary disorder (COPD), asthma, constipation, chronic idiopathic constipation, dry mouth (xerostomia), gum disease, and gastrointestinal problems caused by radiation and chemotherapy for cancer.Type: ApplicationFiled: November 16, 2007Publication date: September 29, 2011Inventors: Efrat Ben-Zeev, Vincent Jacques, Yael Marantz, A. Sekar Reddy, Zhaoda Zhang, Oren Becker, Dilara Mccauley, Pini Orbach, Sharon Shacham, Ashis K. Saha, Michael Xie
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Publication number: 20110236486Abstract: A system and method are provided for controlling an internal combustion engine driving a generator/welder or a stand-alone generator. Controlling the engine may include altering the engine speed based upon a detected demand on the generator and/or operating parameters of a welder. For example, the engine speed may be increased based on a detected draw on the generator and/or the operating parameters of the welder. In addition, the engine speed may be automatically decreased to a non-standard idle speed or the engine may be automatically turned off if no demand is detected for a period of time. Additionally, the engine speed may be increased if only frequency-insensitive demands are detected on the generator. Combinations of these and further methods may be executed. Various devices are provided for implementing the above methods.Type: ApplicationFiled: November 30, 2009Publication date: September 29, 2011Inventors: Gaetano Giammona, Fabio Palumbo, Giovanna Pitarresi
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Publication number: 20110236930Abstract: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).Type: ApplicationFiled: March 8, 2011Publication date: September 29, 2011Inventors: Eliana Saxon, Carolyn Ruth Bertozzi
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Publication number: 20110237527Abstract: The present invention relates to compounds which are inhibitors of sodium dependent glucose co-transporter-2 (SGLT-2). These compounds are used in the treatment of various disorders, including diabetes, impaired glucose tolerance, insulin resistance, retinopathy, nephropathy, neuropathy, cataracts, hyperglycemia, hyperinsulinemia, hyperchlolesterolemia, elevated blood level of free fatty acids or glycerol, hyperlipidemia, hypertriglyceridemia, obesity, wound healing, tissue ischemia, atherosclerosis, and hypertension. These compounds and compositions are also useful for treating and preventing kidney stones, hyperuricemia, gout, and hyponatremia. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: March 21, 2011Publication date: September 29, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Shuang LIU, Cheng GUO, Min HU, Douglas B. KITCHEN, Peter R. GUZZO, Russell DEORAZIO
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Publication number: 20110230403Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts, to formulations and uses of the compounds of formula (I) in the treatment of metabolic disorders.Type: ApplicationFiled: September 17, 2009Publication date: September 22, 2011Applicant: NOVARTIS AGInventors: P. Venkata Palle, Dumbala Srinivas Reddy, Suresh Eknath Kurhade, Debnath Bhuniya
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Publication number: 20110224409Abstract: An amine or hydrazide derivative of a sialic acid unit, e.g. in a polysaccharide, is reacted with a bifunctional reagent at least one of the functionalities of which is an ester of N-hydroxy succinimide, to form an amide or hydrazide product. The product has a useful functionality, which allows it to be conjugated, for instance to proteins, drugs, drug delivery systems or the like. The process is of particular utility for derivatising amine groups introduced in sialic acid terminal groups of polysialic acids.Type: ApplicationFiled: January 10, 2011Publication date: September 15, 2011Inventors: Sanjay JAIN, Ioannis Papaioannou, Smita Thobhani
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Publication number: 20110224156Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: March 8, 2011Publication date: September 15, 2011Inventors: Mark A. Wolf, Keith D. Barnes
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Publication number: 20110217339Abstract: The present invention relates to pharmaceutical compositions which are useful in the treatment of diseases where excess mucus is present in the respiratory tract, such as cystic fibrosis and chronic obstructive pulmonary disease. In particular, the invention relates to pharmaceutical compositions for administration by pulmonary inhalation.Type: ApplicationFiled: March 8, 2011Publication date: September 8, 2011Applicant: Vectura LimitedInventors: David MORTON, David GANDERTON, John STANIFORTH, Yorick KAMLAG
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Publication number: 20110212907Abstract: The present invention relates to novel synthetic hexadecasaccharides with antithrombotic activity, having at least one covalent bond with an amino chain, and to the preparation method thereof and to the therapeutic use thereof.Type: ApplicationFiled: August 24, 2009Publication date: September 1, 2011Applicant: SANOFI-AVENTISInventors: Marie-Claude Rouchon, Joseph Schofield, Dave Smith, Patrick Soubayrol
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Publication number: 20110212917Abstract: Provided are effective and highly safe agents, medicaments and the like for ameliorating various disorders caused by brain hypofunction. Also provided is a preventing or ameliorating agent for brain hypofunction containing N-acetyl-D-mannosamine, a pharmaceutical composition for preventing, ameliorating or treating disorders due to brain hypofunction, containing an effective amount of N-acetyl-D-mannosamine and a pharmaceutically acceptable carrier, and a food comprising N-acetyl-D-mannosamine added thereto.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicants: The University of Tokyo, School Corporation, Azabu Veterinary Medicine Educational InstitutionInventors: Kunio SHIOTA, Masayoshi KUWAHARA, Takefumi KIKUSUI, Shintaro YAGI
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Publication number: 20110206734Abstract: Described herein are fatty acid carbohydrate-hydroxyl-hybrid compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.Type: ApplicationFiled: August 7, 2008Publication date: August 25, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Kevin J. Yarema, Udayanath Aich, Christopher Thomas Campbell, Srinivasa-Gopalan Sampathkumar, Sean S. Choi, Michael Adam Meledeo, Christopher Weier
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Publication number: 20110201794Abstract: Methods are described for the preparation of combinatorial libraries of potentially biologically active disaccharide compounds. These compounds are variously functionalized, with a view to varying lipid solubility size, function an other properties, with the particular aim of discovering novel drug or drug-like compounds, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of disaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of pharmaceutically useful groups and isosteres.Type: ApplicationFiled: December 17, 2010Publication date: August 18, 2011Applicant: Alchemia LimitedInventors: Wim Meutermans, Michael L. West, George Adamson, Giang Thanh Le, Nicholas B. Drinnan, Giovani Abbenante, Bernd Becker, Matthias Grathwohl, Premraj Rajaratnam, Gerald Tometzki
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Patent number: 7993678Abstract: The present invention relates to the modification of hyaluronic acid (HA) with aryl/alkyl succinic anhydrides (ASA) to produce aryl/alkyl succinic anhydride HA derivatives, to the derivatives as such, and to their applications and uses, particularly in the cosmetic and biomedical industries. The ASA-HA derivatives are expected to have interesting properties that can be used for advanced formulation (bind stronger to the skin compared to non-modified HA), possibly also in delivery systems for actives or drugs by encapsulation (nano/micro capsules) or formation of nano/micro spheres. Further, the low MW ASA-HA derivatives are expected to penetrate the skin more efficiently than non-modified HA of the same MW.Type: GrantFiled: August 26, 2006Date of Patent: August 9, 2011Assignee: Novozymes Biopolymer A/SInventors: Kristoffer Tømmeraas, Corinne Eenschooten